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Synonyms: belamaf [4] | belantamab mafodotin-blmf | Blenrep® | GSK-2857916 | GSK2857916
belantamab mafodotin is an approved drug (FDA & EMA (2020))
Compound class:
Antibody
Comment: Belantamab mafodotin (GSK2857916) is a humanised BCMA-targeting antibody-drug conjugate that is in clinical development for multiple myeloma. Mafodotin is the cytotoxic, synthetic antineoplastic monomethyl auristatin F (MMAF; PubChem CID 56841603). Belantamab mafodotin is an IgG1 class antibody so, in addition to its delivery of a cytotoxin, it is predicted to exhibit lytic activity (through complement binding) and/or induce antibody-dependent cell cytotoxicity (ADCC). GlaxoSmithKline claim anti-BCMA ADCs in patent US9273141B2 [1]. SEQ IDs 55 and 63 from US9273141B2 match the full-length heavy chain and light chain sequences respectively, that were submitted to the WHO for the belantamab mafodotin INN.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Algate P, Clegg SJ, Craigen JL, Hamblim PA, Lewis AP, Mayes P, Parmar RS, WattamTAK. (2016)
B cell maturation antigen (BCMA) binding proteins. Patent number: US9273141B2. Assignee: Glaxo Group Ltd. Priority date: 27/05/2011. Publication date: 01/03/2016. |
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2. EMA.
belantamab mafodotin orphan designation, EU/3/17/1925. Accessed on 16/07/2020. Modified on 16/07/2020. ema.europa.eu, https://www.ema.europa.eu/en/medicines/human/orphan-designations/eu3171925 |
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3. Lonial S, Lee HC, Badros A, Trudel S, Nooka AK, Chari A, Abdallah AO, Callander N, Lendvai N, Sborov D et al.. (2020)
Belantamab mafodotin for relapsed or refractory multiple myeloma (DREAMM-2): a two-arm, randomised, open-label, phase 2 study. Lancet Oncol, 21 (2): 207-221. [PMID:31859245] |
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4. Nooka AK, Weisel K, van de Donk NW, Routledge D, Otero PR, Song K, Quach H, Callander N, Minnema MC, Trudel S et al.. (2021)
Belantamab mafodotin in combination with novel agents in relapsed/refractory multiple myeloma: DREAMM-5 study design. Future Oncol, 17 (16): 1987-2003. [PMID:33682447] |
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5. Popat R, Warcel D, O'Nions J, Cowley A, Smith S, Tucker WR, Yong K, Esposti SD. (2020)
Characterization of response and corneal events with extended follow-up after belantamab mafodotin (GSK2857916) monotherapy for patients with relapsed multiple myeloma: a case series from the first-time-in-human clinical trial. Haematologica, 105 (5): e261-e263. [PMID:32107339] |
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6. Trudel S, Lendvai N, Popat R, Voorhees PM, Reeves B, Libby EN, Richardson PG, Anderson Jr LD, Sutherland HJ, Yong K et al.. (2018)
Targeting B-cell maturation antigen with GSK2857916 antibody-drug conjugate in relapsed or refractory multiple myeloma (BMA117159): a dose escalation and expansion phase 1 trial. Lancet Oncol, 19 (12): 1641-1653. [PMID:30442502] |
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7. Trudel S, Lendvai N, Popat R, Voorhees PM, Reeves B, Libby EN, Richardson PG, Hoos A, Gupta I, Bragulat V et al.. (2019)
Antibody-drug conjugate, GSK2857916, in relapsed/refractory multiple myeloma: an update on safety and efficacy from dose expansion phase I study. Blood Cancer J, 9 (4): 37. [PMID:30894515] |
